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Found 605 with Last Name = 'bishop' and Initial = 'a'
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM18771((2S)-2-[(4-{[(2-amino-4-oxo-1,4-dihydroquinazolin-...)
Affinity DataKi:  3.40nMAssay Description:Binding affinity against Thymidylate synthase was measured in vitroMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM50006687((S)-2-(4-(((2-methyl-4-oxo-3,4-dihydroquinazolin-6...)
Affinity DataKi:  10nMAssay Description:Binding affinity against Thymidylate synthase was measured in vitroMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-1(Homo sapiens (Human))
Genzyme

Curated by ChEMBL
LigandPNGBDBM50383265(CHEMBL2032368)
Affinity DataKi:  11nMAssay Description:Inhibition of human Pim-1 using 5-FAM-RSRHSSYPAGT-CONH2 as substrate preincubated for 15 mins prior substrate addition measured after 45 mins by fluo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM50014480((S)-2-(4-(((4-oxo-3,4-dihydroquinazolin-6-yl)methy...)
Affinity DataKi:  27nMAssay Description:Concentration required for in vitro inhibition of thymidylate synthaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Rattus norvegicus (rat))
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM18771((2S)-2-[(4-{[(2-amino-4-oxo-1,4-dihydroquinazolin-...)
Affinity DataKi:  75nMAssay Description:Inhibitory activity against Dihydrofolate reductase in rat liverMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein phosphatase non-receptor type 1(Homo sapiens (Human))
Amherst College

Curated by ChEMBL
LigandPNGBDBM50118792(2-(OXALYL-AMINO)-4,5,6,7-TETRAHYDRO-THIENO[2,3-C]P...)
Affinity DataKi:  230nMAssay Description:Inhibition of PTP1B I219A mutantMore data for this Ligand-Target Pair
TargetTyrosine-protein phosphatase non-receptor type 2(Homo sapiens (Human))
Amherst College

Curated by ChEMBL
LigandPNGBDBM50118792(2-(OXALYL-AMINO)-4,5,6,7-TETRAHYDRO-THIENO[2,3-C]P...)
Affinity DataKi:  710nMAssay Description:Inhibition of TCPTP I220A mutantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein phosphatase non-receptor type 1(Homo sapiens (Human))
Amherst College

Curated by ChEMBL
LigandPNGBDBM50118762(2-(Oxalyl-amino)-4,5,6,7-tetrahydro-benzo[b]thioph...)
Affinity DataKi:  1.00E+3nMAssay Description:Inhibition of PTP1B I219A mutantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Rattus norvegicus (rat))
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM50014480((S)-2-(4-(((4-oxo-3,4-dihydroquinazolin-6-yl)methy...)
Affinity DataKi:  2.25E+3nMAssay Description:Inhibitory activity against Dihydrofolate reductase in rat liverMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDihydrofolate reductase(Rattus norvegicus (rat))
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM50006687((S)-2-(4-(((2-methyl-4-oxo-3,4-dihydroquinazolin-6...)
Affinity DataKi: >2.66E+3nMAssay Description:Inhibitory activity against Dihydrofolate reductase in rat liverMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein phosphatase non-receptor type 1(Homo sapiens (Human))
Amherst College

Curated by ChEMBL
LigandPNGBDBM50118792(2-(OXALYL-AMINO)-4,5,6,7-TETRAHYDRO-THIENO[2,3-C]P...)
Affinity DataKi:  6.00E+3nMAssay Description:Inhibition of wild type PTP1BMore data for this Ligand-Target Pair
TargetTyrosine-protein phosphatase non-receptor type 2(Homo sapiens (Human))
Amherst College

Curated by ChEMBL
LigandPNGBDBM50118792(2-(OXALYL-AMINO)-4,5,6,7-TETRAHYDRO-THIENO[2,3-C]P...)
Affinity DataKi:  1.00E+4nMAssay Description:Inhibition of TCPTPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein phosphatase non-receptor type 1(Homo sapiens (Human))
Amherst College

Curated by ChEMBL
LigandPNGBDBM50187184(2-(carboxyformamido)-5,5,7,7-tetramethyl-4,5,6,7-t...)
Affinity DataKi:  1.00E+4nMAssay Description:Inhibition of PTP1B I219A mutantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein phosphatase non-receptor type 1(Homo sapiens (Human))
Amherst College

Curated by ChEMBL
LigandPNGBDBM50187184(2-(carboxyformamido)-5,5,7,7-tetramethyl-4,5,6,7-t...)
Affinity DataKi:  2.70E+4nMAssay Description:Inhibition of PTP1B V49A mutantMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein phosphatase non-receptor type 1(Homo sapiens (Human))
Amherst College

Curated by ChEMBL
LigandPNGBDBM50118762(2-(Oxalyl-amino)-4,5,6,7-tetrahydro-benzo[b]thioph...)
Affinity DataKi:  3.40E+4nMAssay Description:Inhibition of wild type PTP1BMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein phosphatase non-receptor type 1(Homo sapiens (Human))
Amherst College

Curated by ChEMBL
LigandPNGBDBM50187184(2-(carboxyformamido)-5,5,7,7-tetramethyl-4,5,6,7-t...)
Affinity DataKi: >3.00E+5nMAssay Description:Inhibition of wild type PTP1BMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188514(4,7,7-trimethyl-4-phenyl-3-(trifluoromethyl)-2,4,6...)
Affinity DataIC50:  0.400nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-1(Homo sapiens (Human))
Genzyme

Curated by ChEMBL
LigandPNGBDBM50383272(CHEMBL2032375)
Affinity DataIC50:  0.470nMAssay Description:Inhibition of human Pim-1 using 5-FAM-RSRHSSYPAGT-CONH2 as substrate preincubated for 15 mins prior substrate addition measured after 45 mins by fluo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-1(Homo sapiens (Human))
Genzyme

Curated by ChEMBL
LigandPNGBDBM50345259(CHEMBL1782530 | cis-7-(4-aminocyclohexylamino)-5-b...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human Pim1 using 5-FAM-RSRHSSYPAGT-CONH2 as substrate after 45 mins by off-chip mobility shift methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188512((R)-4-(2-methoxyphenyl)-7,7-dimethyl-3-(trifluorom...)
Affinity DataIC50:  3nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188514(4,7,7-trimethyl-4-phenyl-3-(trifluoromethyl)-2,4,6...)
Affinity DataIC50:  4nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-2(Homo sapiens (Human))
Genzyme

Curated by ChEMBL
LigandPNGBDBM50345259(CHEMBL1782530 | cis-7-(4-aminocyclohexylamino)-5-b...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human Pim2 using 5-FAM-RSRHSSYPAGT-CONH2 as substrate after 90 mins by off-chip mobility shift methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188515((S)-3-cyclopropyl-4,7,7-trimethyl-4-phenyl-2,4,6,7...)
Affinity DataIC50:  5nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lck(Homo sapiens (Human))
Princeton University

LigandPNGBDBM25116(1-tert-butyl-3-(4-methylphenyl)-1H-pyrazolo[3,4-d]...)
Affinity DataIC50:  5nMAssay Description:Inhibition of protein tyrosine kinasesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Fyn(Homo sapiens (Human))
Princeton University

LigandPNGBDBM25116(1-tert-butyl-3-(4-methylphenyl)-1H-pyrazolo[3,4-d]...)
Affinity DataIC50:  6nMAssay Description:Inhibition of protein tyrosine kinasesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188511((S)-3,7,7-Trimethyl-4-(2-(trifluoromethyl)phenyl)-...)
Affinity DataIC50:  7nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM60933((S)-3,4,7,7-tetramethyl-4-phenyl-2,4,6,7,8,9-hexah...)
Affinity DataIC50:  8nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM50014498((S)-2-(4-(((2-amino-4-oxo-3,4-dihydroquinazolin-6-...)
Affinity DataIC50:  9nMAssay Description:Concentration of the compound required to inhibit 50% activity of Thymidylate synthase was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188512((R)-4-(2-methoxyphenyl)-7,7-dimethyl-3-(trifluorom...)
Affinity DataIC50:  10nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188511((S)-3,7,7-Trimethyl-4-(2-(trifluoromethyl)phenyl)-...)
Affinity DataIC50:  11nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM173197(US10137122, Compound 53 | US9096594, 54)
Affinity DataIC50:  12nMT: 2°CAssay Description:The GSK3beta primary screen was conducted in assay ready 1536 plates (Aurora 29847) that contain 2.5 mL/well of 10 mM compound. Human GSK3beta as a G...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM173197(US10137122, Compound 53 | US9096594, 54)
Affinity DataIC50:  13nMT: 2°CAssay Description:The GSK3beta primary screen was conducted in assay ready 1536 plates (Aurora 29847) that contain 2.5 mL/well of 10 mM compound. Human GSK3beta as a G...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188505(4-(2-fluorophenyl)-3,7,7-trimethyl-2,4,6,7,8,9-hex...)
Affinity DataIC50:  18nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-1(Homo sapiens (Human))
Genzyme

Curated by ChEMBL
LigandPNGBDBM50345260(CHEMBL1782531 | trans-7-(4-aminocyclohexylamino)-5...)
Affinity DataIC50:  19nMAssay Description:Inhibition of human Pim1 using 5-FAM-RSRHSSYPAGT-CONH2 as substrate after 45 mins by off-chip mobility shift methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188515((S)-3-cyclopropyl-4,7,7-trimethyl-4-phenyl-2,4,6,7...)
Affinity DataIC50:  19nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM50006689((S)-2-(2-fluoro-4-(((2-methyl-4-oxo-3,4-dihydroqui...)
Affinity DataIC50:  20nMAssay Description:Inhibition of thymidylate synthase from L1210 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-1(Homo sapiens (Human))
Genzyme

Curated by ChEMBL
LigandPNGBDBM50345250(5-bromo-7-(piperidin-4-ylmethylamino)benzofuran-2-...)
Affinity DataIC50:  20nMAssay Description:Inhibition of human Pim1 using 5-FAM-RSRHSSYPAGT-CONH2 as substrate after 45 mins by off-chip mobility shift methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM50006689((S)-2-(2-fluoro-4-(((2-methyl-4-oxo-3,4-dihydroqui...)
Affinity DataIC50:  20nMAssay Description:Inhibition of partially purified thymidylate synthase (TS)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM18771((2S)-2-[(4-{[(2-amino-4-oxo-1,4-dihydroquinazolin-...)
Affinity DataIC50:  20nMAssay Description:Concentration of the compound required to inhibit 50% activity of Thymidylate synthase was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM50006689((S)-2-(2-fluoro-4-(((2-methyl-4-oxo-3,4-dihydroqui...)
Affinity DataIC50:  20nMAssay Description:Concentration of the compound required to inhibit 50% activity of Thymidylate synthase was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM18771((2S)-2-[(4-{[(2-amino-4-oxo-1,4-dihydroquinazolin-...)
Affinity DataIC50:  20nMAssay Description:In vitro inhibitory activity against thymidylate synthase (TS) from L1210 mouse leukemia cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM18771((2S)-2-[(4-{[(2-amino-4-oxo-1,4-dihydroquinazolin-...)
Affinity DataIC50:  20nMAssay Description:Concentration required for in vitro inhibition of thymidylate synthaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-2(Homo sapiens (Human))
Genzyme

Curated by ChEMBL
LigandPNGBDBM50345245(CHEMBL1782516 | trans-5-(6-(4-(aminomethyl)cyclohe...)
Affinity DataIC50:  21nMAssay Description:Inhibition of human Pim2 using 5-FAM-RSRHSSYPAGT-CONH2 as substrate after 90 mins by off-chip mobility shift methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM50004387(2-{4-[(2,4-Dichloro-quinolin-6-ylmethyl)-prop-2-yn...)
Affinity DataIC50:  23nMAssay Description:In vitro inhibitory activity against thymidylate synthase from L1210 mouse leukemia cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-1(Homo sapiens (Human))
Genzyme

Curated by ChEMBL
LigandPNGBDBM26626((5Z)-5-{[3-(trifluoromethyl)phenyl]methylidene}-1,...)
Affinity DataIC50:  24nMAssay Description:Inhibition of human Pim-1 using 5-FAM-RSRHSSYPAGT-CONH2 as substrate preincubated for 15 mins prior substrate addition measured after 45 mins by fluo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM60933((S)-3,4,7,7-tetramethyl-4-phenyl-2,4,6,7,8,9-hexah...)
Affinity DataIC50:  26nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM172196(US9090564, 10 | US9096594, 22)
Affinity DataIC50:  27nMT: 2°CAssay Description:The GSK3beta primary screen was conducted in assay ready 1536 plates (Aurora 29847) that contain 2.5 mL/well of 10 mM compound. Human GSK3beta as a G...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188509(BRD3937 | US10137122, Compound 22)
Affinity DataIC50:  28nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM188508(3,7,7-Trimethyl-4-(o-tolyl)-2,4,6,7,8,9-hexahydro-...)
Affinity DataIC50:  32nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetThymidylate synthase(Mus musculus)
Ici Pharmaceuticals Group

Curated by ChEMBL
LigandPNGBDBM50014496((S)-2-(2-fluoro-4-(((2-methoxy-4-oxo-3,4-dihydroqu...)
Affinity DataIC50:  36nMAssay Description:Concentration of the compound required to inhibit 50% activity of Thymidylate synthase was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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